| Summary: | In this work we present the microwave-assisted synthesis and in vitro acetylcholinesterase inhibition of a series of new caffeine derivatives. The design of these new compounds was inspired by the caffeine–pyrrolidine hybrids that act as AChE inhibitors and nAChR activators, previously reported by our group. All of the new caffeine analogs inhibited AChE. Among them, the compound <b>2b</b> (1,3-dimethyl-7-(6-(piperidin-1-yl)hexyl)-3,7-dihydro-1H-purine-2,6-dione) showed the strongest effect (IC<sub>50</sub> = 0.17 µM) on AChE, with higher potency than caffeine–pyrrolidine hybrids. These preliminary studies suggest that these new compounds might be interesting multifunctional drugs destined to stimulate cholinergic signage.
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